PE20000756A1 - GONADOTROPIN RELEASING HORMONE ANTAGONISTS - Google Patents

GONADOTROPIN RELEASING HORMONE ANTAGONISTS

Info

Publication number
PE20000756A1
PE20000756A1 PE1999000683A PE00068399A PE20000756A1 PE 20000756 A1 PE20000756 A1 PE 20000756A1 PE 1999000683 A PE1999000683 A PE 1999000683A PE 00068399 A PE00068399 A PE 00068399A PE 20000756 A1 PE20000756 A1 PE 20000756A1
Authority
PE
Peru
Prior art keywords
alkyl
heterocycle
members
releasing hormone
gonadotropin releasing
Prior art date
Application number
PE1999000683A
Other languages
Spanish (es)
Inventor
Michael H Fisher
Mark Goulet
Wallace T Ashton
Lin Chu
Jonathan Young
Peter Lin
Mitre M Ponpipom
Matthew J Wyvratt
Narindar N Girotra
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20000756A1 publication Critical patent/PE20000756A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Abstract

SE REFIERE A UN COMPUESTO DERIVADO DE INDOL (I); A ES ALQUILO C1-C6, ALQUENILO C3-C6, ENTRE OTROS; RO ES H, ALQUILO C1-C6; R1 ES UN GRUPO a, b, c, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, ENTRE OTROS; R2 Y A FORMAN UN ANILLO DE 5-7 MIEMBROS; R3, R4 Y R5 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R3 Y R4 FORMAN UN ANILLO DE 3-7 MIEMBROS, HETEROCICLO; R6 ES H, ALQUILO C1-C6, ARILO, ENTRE OTROS; R7 ES H, ALQUILO C1-C6; CUANDO X ES H o HALOGENO, R7 NO SE PRESENTA; R8 ES COOR20, CONR20R21, ENTRE OTROS; R7 Y R8 FORMAN UN HETEROCICLO; R9 Y R9a SON H, ALQUILO C1-C6, ENTRE OTROS; R9 Y R9a o R10 Y R10a FORMAN UN CARBOCICLO DE 3-7 MIEMBROS, =O; R9 Y A FORMAN UN HETEROCICLO DE 3-7 MIEMBROS; R10 Y R10a SON H, ALQUILO C1-C6, ARILO, ENTRE OTROS; R9 Y R10 FORMAN UN CARBOCICLO DE 3-7 MIEMBROS, HETEROCICLO; R9 Y R2; R10 Y R2; R10 Y A FORMAN UN HETEROCICLO C3-C7; R11 Y R12 SON H, ALQUILO C1-C6, ENTRE OTROS; R20 Y R21 SON H, ALQUILO C1-C6, ENTRE OTROS; X ES N, O, SOn, CO, C(R11R12)p; Z ES O, S, NR11; m ES 0-3; n ES 0-2; p ES 0-4. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS UN COMPUESTO QUE TIENE ACTIVIDAD DE HORMONA LIBERADORA DE LA HORMONA LUTEINIZANTE. EL COMPUESTO I INHIBE A LA HORMONA LIBERADORA DE GONADOTROPINA Y PUEDE SER UTIL PARA EL TRATAMIENTO DE CANCER DEPENDIENTE DE HORMONAS SEXUALES, HIPERTROFIA PROSTATICA BENIGNAREFERS TO A COMPOUND DERIVED FROM INDOL (I); A IS C1-C6 ALKYL, C3-C6 ALKYL, AMONG OTHERS; RO IS H, C1-C6 ALKYL; R1 IS A GROUP a, b, c, AMONG OTHERS; R2 IS H, C1-C6 ALKYL, AMONG OTHERS; R2 AND A FORM A RING OF 5-7 MEMBERS; R3, R4 AND R5 ARE H, C1-C6 ALKYL, C2-C6 ALKYL, AMONG OTHERS; R3 AND R4 FORM A RING OF 3-7 MEMBERS, HETEROCICLO; R6 IS H, C1-C6 ALKYL, ARYL, AMONG OTHERS; R7 IS H, C1-C6 ALKYL; WHEN X IS H or HALOGEN, R7 IS NOT PRESENTED; R8 IS COOR20, CONR20R21, AMONG OTHERS; R7 AND R8 FORM A HETEROCYCLE; R9 AND R9a ARE H, C1-C6 ALKYL, AMONG OTHERS; R9 AND R9a or R10 AND R10a FORM A 3-7 MEMBER CARBOCYCLE, = O; R9 AND A FORM A HETEROCYCLE OF 3-7 MEMBERS; R10 AND R10a ARE H, C1-C6 ALKYL, ARYL, AMONG OTHERS; R9 AND R10 FORM A CARBOCYCLE OF 3-7 MEMBERS, HETEROCYCLE; R9 and R2; R10 and R2; R10 AND A FORM A C3-C7 HETEROCYCLE; R11 AND R12 ARE H, C1-C6 ALKYL, AMONG OTHERS; R20 AND R21 ARE H, C1-C6 ALKYL, AMONG OTHERS; X IS N, O, SOn, CO, C (R11R12) p; Z IS O, S, NR11; m IS 0-3; n IS 0-2; p IS 0-4. IT ALSO REFERS TO A COMPOSITION THAT ALSO INCLUDES A COMPOUND THAT HAS LUTEINIZING HORMONE-RELEASING HORMONE ACTIVITY. COMPOUND I INHIBITES GONADOTROPIN RELEASING HORMONE AND MAY BE USEFUL FOR THE TREATMENT OF SEXUAL HORMONE-DEPENDENT CANCER, BENIGN PROSTATIC HYPERTROPHY

PE1999000683A 1998-07-14 1999-07-09 GONADOTROPIN RELEASING HORMONE ANTAGONISTS PE20000756A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/115,497 US6200957B1 (en) 1995-12-14 1998-07-14 Antagonists of gonadotropin releasing hormone

Publications (1)

Publication Number Publication Date
PE20000756A1 true PE20000756A1 (en) 2000-08-30

Family

ID=22361786

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1999000683A PE20000756A1 (en) 1998-07-14 1999-07-09 GONADOTROPIN RELEASING HORMONE ANTAGONISTS

Country Status (10)

Country Link
US (1) US6200957B1 (en)
EP (1) EP1095038B1 (en)
JP (1) JP2002520409A (en)
AT (1) ATE248832T1 (en)
AU (1) AU760030B2 (en)
CA (1) CA2337407A1 (en)
DE (1) DE69911023T2 (en)
ES (1) ES2205855T3 (en)
PE (1) PE20000756A1 (en)
WO (1) WO2000004013A1 (en)

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GB0022670D0 (en) 2000-09-15 2000-11-01 Astrazeneca Ab Molecules
SE0100566D0 (en) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
SE0101692D0 (en) 2001-05-14 2001-05-14 Astrazeneca Ab Compounds
AU2002351468A1 (en) * 2001-10-09 2003-05-12 Oregon Health And Science University Rescue of gonadotropin releasing hormone receptor mutants
AU2003202115A1 (en) 2002-02-12 2003-09-04 Pfizer Inc. Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh)
AU2003233127A1 (en) 2002-06-13 2003-12-31 Pfizer Inc. Non-peptide gnrh agents, pharmaceutical compositions and methods for their use
TW200413351A (en) 2002-08-21 2004-08-01 Astrazeneca Ab Chemical compounds
AU2003267551A1 (en) 2002-08-21 2004-03-11 Astrazeneca Ab Thieno-pyrrole compounds as antagonists of gonadotropin releasing hormone
US7253290B2 (en) 2002-08-21 2007-08-07 Astrazeneca Ab Pyrazole derivatives as GnRH inhibitors
TW200407127A (en) 2002-08-21 2004-05-16 Astrazeneca Ab Chemical compounds
GB0219472D0 (en) 2002-08-21 2002-10-02 Astrazeneca Ab Chemical compounds
US7045527B2 (en) 2002-09-24 2006-05-16 Amgen Inc. Piperidine derivatives
DE102004033902A1 (en) 2004-07-14 2006-02-16 Zentaris Gmbh New tetrahydrocarbazole compounds are neurokinin-1 receptor antagonists useful to treat or prevent e.g. pubertas praecox, hirsutism, polycystic ovary syndrome, hormone dependent neoplastic diseases and Alzheimer's disease
EP2095818A1 (en) 2008-02-29 2009-09-02 AEterna Zentaris GmbH Use of LHRH antagonists at non-castrating doses
WO2015007606A1 (en) * 2013-07-15 2015-01-22 Bayer Pharma Aktiengesellschaft Spiroindoline derivatives and pharmaceutical compositions thereof
WO2015091315A1 (en) * 2013-12-19 2015-06-25 Bayer Pharma Aktiengesellschaft Spiro[indolin-3,4'-piperidine] derivatives as gnrh receptor antagonists
WO2018002673A1 (en) 2016-07-01 2018-01-04 N4 Pharma Uk Limited Novel formulations of angiotensin ii receptor antagonists
AU2018249675B2 (en) 2017-04-06 2021-08-19 Inventiva New compounds inhibitors of the YAP/TAZ-TEAD interaction and their use in the treatment of malignant mesothelioma.
EP3632908A1 (en) 2018-10-02 2020-04-08 Inventiva Inhibitors of the yap/taz-tead interaction and their use in the treatment of cancer

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US4678784A (en) 1984-04-11 1987-07-07 Mcneilab, Inc. Method for the treatment of LHRH diseases and conditions
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Also Published As

Publication number Publication date
DE69911023T2 (en) 2004-06-03
EP1095038A1 (en) 2001-05-02
WO2000004013A1 (en) 2000-01-27
JP2002520409A (en) 2002-07-09
AU4981699A (en) 2000-02-07
ES2205855T3 (en) 2004-05-01
EP1095038B1 (en) 2003-09-03
AU760030B2 (en) 2003-05-08
ATE248832T1 (en) 2003-09-15
US6200957B1 (en) 2001-03-13
CA2337407A1 (en) 2000-01-27
DE69911023D1 (en) 2003-10-09

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Legal Events

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